Molecular design and structure–activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664
…, CY Chang, S Chong, DB Wang-Iverson…
文献索引：Das, Jagabandhu; Kimball; Hall, Steven E.; Han, Wen-Ching; Iwanowicz, Edwin; Lin, James; Moquin, Robert V.; Reid, Joyce A.; Sack, John S.; Malley, Mary F.; Chang, Chiehying Y.; Chong, Saeho; Wang-Iverson, David B.; Roberts, Daniel G.M.; Seiler, Steven M.; Schumacher, William A.; Ogletree, Martin L. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 1 p. 45 - 49
A series of structurally novel small molecule inhibitors of human α-thrombin was prepared to elucidate their structure–activity relationships (SARs), selectivity and activity in vivo. BMS- 189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human α-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.
